CN106667917A - Faropenem sodium granules - Google Patents
Faropenem sodium granules Download PDFInfo
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- CN106667917A CN106667917A CN201510782830.9A CN201510782830A CN106667917A CN 106667917 A CN106667917 A CN 106667917A CN 201510782830 A CN201510782830 A CN 201510782830A CN 106667917 A CN106667917 A CN 106667917A
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- faropenem
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- sodium
- faropenem sodium
- mannitol
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Abstract
The invention provides faropenem sodium granules. The faropenem sodium granules are characterized by being prepared from the following components in parts by weight: 100 parts of faropenem sodium calculated on the basis of faropenem, 300 to 400 parts of saccharose, 400 to 575 parts of mannitol, 8.0 to 80 parts of hydroxypropyl methylcellulose, 0.1 to 0.2 part of sodium calcium edentate, 0 to 50 parts of a taste correcting agent and 0 to 0.2 part of a color correcting agent. The prepared faropenem sodium granules have good granule hardness, high water solubility and moderate taste and color, solve the defect of low stability of the conventional granules, and are stable in release, durable in action, stable in curative effect, small in toxic and side effect and particularly favorable for children and people suffering from dysphagia to take.
Description
Technical field
The present invention relates to a kind of solid pharmaceutical preparation, specifically, is related to a kind of Faropenem sodium granule.Belong to pharmaceutical preparation
Field.
Background technology
Faropenem sodium (Faropenem Sodium) is the beta-lactam antibiotic of penemss, in being such medicine
, the orally available broad ectrum antibiotic stable to beta-lactamase of first listing.The same, the method with other beta-lactam antibiotics
Faropenem plays bactericidal action by suppressing the synthesis of bacteria cell wall.The medical instrument has very strong antibacterial activity, especially to golden Portugal
The antibacterial activity of the anaerobe such as gram positive bacteria and bacteroides fragilises such as bacterium, penicillin-fast streptococcus pneumoniae, streptococcus faecalis is obvious
Better than existing cephalosporin, such as cefoxitin ester, cefteram, cefixime, cefaclor.Anti- gram negative bacteria
Activity is similar to oral cephalosporin, and anti Bacillus pyocyaneu Flugge effect is weaker.This product is stable to beta-lactamase, to resistance to cephalosporin
Citrobacter freundii, enterobacter cloacae etc. also have preferable antibacterial action.
Faropenem sodium is the strong antibiotic of new generation of good safety, has a broad antifungal spectrum, antimicrbial power.Faropenem sodium is to temperature
Degree and humidity less stable, easily polymerization, produce high molecular polymer, cause anaphylaxiss, therefore, control its polyphosphazene polymer
The content of compound, the quality to controlling product is extremely important.At present clinically the oral formulations of Faropenem sodium are of less types,
Need to three times a day take, have a strong impact on the Clinical practice and patient's medication adaptability of faropenem.
Compare tablet and capsule, and taking for granule is easily received by child and the crowd for having dysphagia, however,
Again generally existing preparation stability is poor for existing faropenem granule, about the problem that material substantially increases.
The content of the invention
For convenience of the application of clinically Faropenem sodium, for patient provide it is a kind of safely, effectively, the Fa Luopei of taking convenience
Southern preparation of sodium, the present invention is designed and there is provided a kind of Faropenem sodium granule, and it has slow releasing function and with preferable quality
Stability.Technical solution of the present invention is as follows：
The invention provides a kind of Faropenem sodium granule, it is characterised in that be made up of the component of following weight portion：With Fa Luopei
100 parts of the Faropenem sodium that south calculates, sucrose 300-400 parts, Mannitol 400-575 part, hypromellose 8.0-80 parts,
Calcium disodium edetate 0.1-0.2 parts, correctivess 0-50 parts rectify toner 0-0.2 parts.
Preferably, present invention Faropenem sodium granule described above, it is characterised in that be made up of the component of following weight portion：
With faropenem calculate 100 parts of Faropenem sodium, 300 parts of sucrose, 575 parts of Mannitol, 0.8 part of hypromellose,
0.2 part of calcium disodium edetate, 0.2 part of correctivess rectify 0.16 part of toner.
Wherein, correctivess described above, strong toner, have no particular limits, and can be correctivess commonly used in the art
Or strong toner, such as correctivess can be selected from saccharin sodium, aspartame, stevioside, sucralose etc.；Strong toner can be with
Selected from lemon yellow, the red, sunset yellow of sunset etc..
As one of embodiment of the invention, there is provided a kind of described Faropenem sodium granule, it is characterised in that by such as
Lower component makes 1000 bags：
Preferably, Faropenem sodium granule described above, it is characterised in that method as follows is made：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium, calcium disodium edetate sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
The Faropenem sodium granule of the present invention, by from specific adjuvant, particularly from specific filler sucrose and manna
Alcohol mixture, from specific stabilizer hypromellose and specific chelating agent calcium disodium edetate, through specific proportioning,
Obtained Faropenem sodium granule, not only pellet hardness is preferable, and water solublity is good, and mouthfeel, color and luster are moderate, granule
Aqueous stability is good, solves the defect of existing granule stability difference.
Additionally, the Faropenem sodium granule of the present invention is compared with existing plain particles agent, this preparation only needs be administered once for one day,
Steady release, persistent, stable curative effect, toxic and side effects are little；And compared with the slow releasing preparation of other dosage forms, particle slow release agent
Type is more favorable to child and takes with the patient for having dysphagia.
Specific embodiment
Present invention is explained further and illustrated below by way of specific embodiment, but it is not constituted to the scope of the present invention
Restriction.
Embodiment 1：
Prescription (specification：0.1g)：
Preparation technology：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium, calcium disodium edetate sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Embodiment 2：
Prescription (specification：0.1g)：
Preparation technology：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium, calcium disodium edetate, fragrant citrus essence sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, sunset yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Embodiment 3：
Prescription (specification：0.1g)：
Preparation technology：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, aspartame, calcium disodium edetate sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Comparative example 1：
Prescription (specification：0.1g)：
Preparation technology：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium, calcium disodium edetate sieve；
(2), by step (1) component mix homogeneously；
(3), hydroxyl methylcellulose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Comparative example 2：
Prescription (specification：0.1g)：
Preparation technology：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Embodiment 4 is for the drug release determination of obtained Faropenem sodium granule
With common commercially available Faropenem sodium granule as a comparison, Faropenem sodium particulate samples 1 obtained in Example 1,2,3,
2nd, 3, and each 500mg of Faropenem sodium granule prepared by comparative example 1 and 2, determined with Rotating shaker, with 900mL purification
Water is release medium, and temperature is 37 ± 0.5 DEG C, and rotating speed is 100r/min.Respectively 0.5,1.0,1.5,2.0,4.0,
6.0th, 8.0,10.0,12.0h takes 2.0mL dissolution fluids, contains with reference to second middle Faropenem sodium of Chinese Pharmacopoeia 2015 edition
Quantity measuring method, calculates Faropenem sodium granule in the drug accumulation release rate Q of different time points, is shown in Table 1.
The release in vitro result (Q/%) of the Faropenem sodium granule of table 1
Dissolution test proves that compared with existing plain particles agent, this preparation can put down the Faropenem sodium granule of the present invention
Steady release, persistent, it is possible to reduce medicining times, the patient for being more beneficial for child and having dysphagia takes.This is reached
The prominent technique effect of invention.And comparative example 1 and the difference of sample 1 are only to have changed hypromellose into hydroxypropylcellulose,
Its releasing effect does not just reach completely the steady and lasting effect of the present invention；Likewise, the difference of comparative example 2 and sample 1 is only
It is to eliminate calcium disodium edetate, though its release relatively persistently can occur a large amount of releases, without the present invention in 1.5-2 hours
Stable releasing effect, safety is poor.
Embodiment 5 carries out stability test for obtained Faropenem sodium granule.
With reference to two annex XIX C medicine stability test guidelines of Chinese Pharmacopoeia 2015 edition, the sample provided the present invention
Product 1,2,3 and common commercially available Faropenem sodium granule, and Faropenem sodium granule prepared by comparative example 1 and 2 carries out respectively shadow
Factorial experimentss, accelerated test and long term test are rung, part test result is as shown in the table：
Faropenem sodium granule (sample 1) the influence factor's result of the test of table 2
Remarks：RH：Humidity.
Sample, commercially available plain particles agent and the acceleration of comparative example and long-term test results that the present invention of table 3 is provided
Jing influence factors test, acceleration are tested for 6 months, the investigation of long-term 36 months, commercially available common faropenem granule
Substantially increase with the impurity of comparative example 1-2, stability is remarkably decreased, and the three of the present invention batches of sample indices and 0 month
Relatively, have no significant change.Wherein, obtained by embodiment 1 sample stability is optimum.
Stability test proves the Faropenem sodium granule obtained by the present invention, and not only pellet hardness is preferable, and stability is good
It is good, solve the defect of existing granule stability difference.The technique effect of protrusion of the present invention is reached.
Claims (6)
1. a kind of Faropenem sodium granule, it is characterised in that be made up of the component of following weight portion：With the faropenem that faropenem is calculated
100 parts of sodium, sucrose 300-400 parts, Mannitol 400-575 part, hypromellose 8.0-80 parts, calcium disodium edetate 0.1-0.2
Part, correctivess 0-50 parts rectify toner 0-0.2 parts.
2. Faropenem sodium granule according to claim 1, it is characterised in that be made up of the component of following weight portion：With Fa Luopei
100 parts of the Faropenem sodium that south calculates, sucrose 300-350 parts, Mannitol 500-575 part, hypromellose 8.0-20
Part, 0.2 part of calcium disodium edetate, 0.2 part of correctivess rectify 0.16 part of toner.
3. the Faropenem sodium granule according to claim 1-2, it is characterised in that described correctivess can selected from saccharin sodium,
Aspartame, stevioside, sucralose etc..
4. the Faropenem sodium granule according to claim 1-3, it is characterised in that described strong toner can selected from lemon yellow,
Sunset is red, sunset yellow etc..
5. the Faropenem sodium granule according to claim 1-4, it is characterised in that make 1000 bags by following component：
6. Faropenem sodium granule according to claim 5, it is characterised in that method as follows is made：
(1), Faropenem sodium is pulverized and sieved, sucrose, Mannitol, saccharin sodium, calcium disodium edetate sieve；
(2), by step (1) component mix homogeneously；
(3), hypromellose, lemon yellow are dissolved in into wiring solution-forming in 50% ethanol；
(4), step (2) resulting material is added into the made solution of step (3), mix homogeneously and wet granular processed；
(5), after 35 DEG C～40 DEG C drying under reduced pressure of the made wet granular of step (4), Jing after granulate, packaging is obtained final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510782830.9A CN106667917A (en) | 2015-11-10 | 2015-11-10 | Faropenem sodium granules |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510782830.9A CN106667917A (en) | 2015-11-10 | 2015-11-10 | Faropenem sodium granules |
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| CN106667917A true CN106667917A (en) | 2017-05-17 |
Family
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| CN201510782830.9A Pending CN106667917A (en) | 2015-11-10 | 2015-11-10 | Faropenem sodium granules |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111202714A (en) * | 2020-02-26 | 2020-05-29 | 江苏艾立康药业股份有限公司 | Faropenem sodium particles and preparation method thereof |
| CN113750053A (en) * | 2021-10-28 | 2021-12-07 | 江苏睿实生物科技有限公司 | Faropenem sodium particles and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669943A (en) * | 2008-09-09 | 2010-03-17 | 深圳高卓药业有限公司 | Oral solid preparation of faropenem and salt derivative thereof |
-
2015
- 2015-11-10 CN CN201510782830.9A patent/CN106667917A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101669943A (en) * | 2008-09-09 | 2010-03-17 | 深圳高卓药业有限公司 | Oral solid preparation of faropenem and salt derivative thereof |
Non-Patent Citations (1)
| Title |
|---|
| 姚静编: "《药用辅料应用指南》", 31 August 2011, 中国医药科技出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111202714A (en) * | 2020-02-26 | 2020-05-29 | 江苏艾立康药业股份有限公司 | Faropenem sodium particles and preparation method thereof |
| CN113750053A (en) * | 2021-10-28 | 2021-12-07 | 江苏睿实生物科技有限公司 | Faropenem sodium particles and preparation method thereof |
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